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Fragment-based discovery of selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase PtpA

The development of low μM inhibitors of the Mycobacterium tuberculosis phosphatase PtpA is reported. The most potent of these inhibitors (K(i) = 1.4 ± 0.3 μM) was found to be selective when tested against a panel of human tyrosine and dual-specificity phosphatases (11-fold vs the highly homologous H...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: Rawls, Katherine A., Lang, P. Therese, Takeuchi, Jun, Imamura, Shinichi, Baguley, Tyler D., Grundner, Christoph, Alber, Tom, Ellman, Jonathan A.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2009
Schlagworte:
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC2801607/
https://ncbi.nlm.nih.gov/pubmed/19889539
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2009.10.090
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